Global Patent Index - EP 2873663 A1

EP 2873663 A1 2015-05-20 - Novel uncharged reactivators against OP-inhibition of human acetylcholinesterase

Title (en)

Novel uncharged reactivators against OP-inhibition of human acetylcholinesterase

Title (de)

Neue ungeladenen Reaktivatoren gegen die OP-Hemmung der humanen Acetylcholinesterase

Title (fr)

Nouveaux réactivateurs non chargées contre l'inhibition-OP de l'acétylcholinestérase humaine

Publication

EP 2873663 A1 (EN)

Application

EP 13306584 A

Priority

EP 13306584 A

Abstract (en)

The present invention deals with novel uncharged reactivators of human acetylcholinesterase of formula (II) below, pharmaceutical compositions comprising said compounds, and their use for reactivating human acetylcholinesterase inhibited by at least one organophosphorus nerve agent.

IPC 8 full level

C07D 401/12 (2006.01); A61K 31/473 (2006.01); A61P 25/00 (2006.01)

CPC

C07D 401/12 (2013.01)

Citation (applicant)

  • HESS, B.; KUTZNER, C.; VAN DER SPOEL, D.; LINDAHL, E. J., CHEM. THEORY COMPUT., vol. 4, 2008, pages 435 - 447
  • HORNAK, V.; ABEL, R.; OKUR, A.; STROCKBINE, B.; ROITBERG, A.: "Simmerling, C.", PROTEINS, vol. 65, 2006, pages 712 - 725
  • WANG, J.; WOLF, R. M.; CALDWELL, J. W.; KOLLMAN, P. A.; CASE, D. A., J. COMPUT. CHEM., vol. 25, 2004, pages 1157 - 1174
  • BERENDSEN, H. J. C.; POSTMA, J. P. M.; VAN GUNSTEREN, W. F.; DINOLA, A.; HAAK, J. R. J., CHEM. PHYS., vol. 81, 1984, pages 3684
  • HESS, B.; BEKKER, H.; BERENDSEN, H. J. C.; FRAAIJE, J. G. E. M., J. COMPUT. CHEM., vol. 18, 1997, pages 1463

Citation (search report)

  • [A] GUILLAUME MERCEY ET AL: "Phenyltetrahydroisoquinoline-Pyridinaldoxime Conjugates as Efficient Uncharged Reactivators for the Dephosphylation of Inhibited Human Acetylcholinesterase", JOURNAL OF MEDICINAL CHEMISTRY, vol. 55, no. 23, 13 December 2012 (2012-12-13), pages 10791 - 10795, XP055099217, ISSN: 0022-2623, DOI: 10.1021/jm3015519
  • [A] FEI MAO ET AL: "O-Hydroxyl- or o-amino benzylamine-tacrine hybrids: Multifunctional biometals chelators, antioxidants, and inhibitors of cholinesterase activity and amyloid-[beta] aggregation", BIOORGANIC & MEDICINAL CHEMISTRY, vol. 20, no. 19, 1 October 2012 (2012-10-01), pages 5884 - 5892, XP055099195, ISSN: 0968-0896, DOI: 10.1016/j.bmc.2012.07.045
  • [A] PAWE SZYMASKI ET AL: "Synthesis and biological activity of derivatives of tetrahydroacridine as acetylcholinesterase inhibitors", BIOORGANIC CHEMISTRY, vol. 39, no. 4, 2011 - 2011, pages 138 - 142, XP028296972, ISSN: 0045-2068, [retrieved on 20110512], DOI: 10.1016/J.BIOORG.2011.05.001
  • [A] CARLIER P R ET AL: "Heterodimeric tacrine-based acetylcholinesterase inhibitors: investigating ligand-peripheral site interactions", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY, US, vol. 42, no. 20, 7 October 1999 (1999-10-07), pages 4225 - 4231, XP002434602, ISSN: 0022-2623, DOI: 10.1021/JM990224W

DCS

AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR

Designated extension state (EPC)

BA ME

DOCDB simple family

EP 2873663 A1 20150520; CA 2930895 A1 20150528; EP 3071558 A1 20160928; JP 2017500291 A 20170105; US 2016272620 A1 20160922; WO 2015075082 A1 20150528